Proteinase activated receptor 2: Role of extracellular loop 2 for ligand-mediated activation

British Journal of Pharmacology

Volumn 128, Issue 5, 1999, Pages 1105-1113

  Al Ani, Bahjat ^a   Saifeddine, Mahmoud ^a   Kawabata, Atsufumi ^a,b   Hollenberg, Morley D ^a  

^a UNIVERSITY OF CALGARY   (Canada)

^b KINKI UNIVERSITY   (Japan)

Author keywords

PAR; PAR1; PAR2; Proteinase; Proteinase activated receptor; Trypsin

Indexed keywords

LIGAND; PROTEINASE; RECEPTOR; TRYPSIN;

ANIMAL CELL; ARTICLE; CELL LINE; KIDNEY CELL; NONHUMAN; PRIORITY JOURNAL; RAT;

AMINO ACID SEQUENCE; ANIMALS; BIOTRANSFORMATION; CALCIUM SIGNALING; CELL LINE; EXTRACELLULAR SPACE; FLUORESCENT DYES; LIGANDS; MOLECULAR SEQUENCE DATA; MUTATION; RATS; RECEPTOR, PAR-2; RECEPTORS, THROMBIN; SPECTROMETRY, FLUORESCENCE; TRYPSIN;

EID: 0032712580     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0702834     Document Type: Article

References (30)

1. 2 in rat vascular and gastric smooth muscle. Can. J. Physiol. Pharmacol., 73, 1203-1207.
2. 2-derived peptide ligands. J. Pharmacol. Exp. Ther., in press.
3. BLACKHART, B.D., EMILSSON, K., NGUYEN, D., TENG, W., MARTELLI, A.J., NYSTEDT, S., SUNDELIN, J. & SCARBOROUGH, R.M. (1996). Ligand cross-reactivity within the protease-activated receptor family. J. Biol. Chem., 271, 16466-16471.
4. BÖHM, S.K., KONG, W., BRÖMME, D., SMEEKENS, S.P., ANDERSON, D.C., CONNOLLY, A., KAHN, M., NELKEN, N.A., COUGHLIN, S.R., PAYAN, D.G. & BUNNETT, N.W. (1996). Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2. Biochem. J., 314, 1009-1016.
5. CHAO, B.H., KALKUNTE, S., MARAGANORE, J.M. & STONE, S.R. (1992). Essential groups in synthetic agonist peptides for activation of the platelet thrombin receptor. Biochemistry, 31, 6175-6178.
6. CHEN, J., ISHII, M., WANG, L., ISHII, K. & COUGHLIN, S.R. (1994). Thrombin receptor activation. Confirmation of the intramolecular tethered liganding hypothesis and discovery of an alternative intermolecular liganding mode. J. Biol. Chem., 269, 16041-16045.
7. DERY, O., CORVERA, C.U., STEINHOFF, M. & BUNNETT, N.W. (1998). Proteinase-activated receptors: novel mechanisms of signaling by serine proteases. Am. J. Physiol., 274, 1429-1452.
8. GERSZTEN, R.E., CHEN, J., ISHII, M., ISHII, K., WANG, L., NANEVICZ, T., TURCK, C.W., VU, T K. & COUGHLIN, S.R. (1994). Specificity of the thrombin receptor for agonist peptide is defined by its extracellular surface. Nature, 368, 648-651.
9. HOLLENBERG, M.D., LANIYONU, A.A., SAIFEDDINE, M. & MOORE, G.J. (1993). Role of the amino-and carboxyl-terminal domains of thrombin receptor-derived polypeptides in biological activity in vascular endothelium and gastric smooth muscle: evidence for receptor subtypes. Mol. Pharmacol., 43, 921-930.
10. HOLLENBERG, M D., SAIFEDDINE, M. & AL-ANI, B. (1996). Proteinase-activated receptor-2 in rat aorta: structural requirements for agonist activity of receptor-activating peptides. Mol. Pharmacol., 49, 229-233.
11. HOLLENBERG, M.D., SAIFEDDINE, M., AL-ANI, B. & KAWABATA, A. (1997). Proteinase-activated receptors: structural requirements for activity, receptor cross-reactivity and receptor selectivity of receptor-activating peptides. Can. J. Phys. Pharmacol., 75, 832-841.
12. HOLLENBERG, M.D., YANG, S.G., LANIYONU, A.A., MOORE, G.J. & SAIFEDDINE, M. (1992). Action of thrombin receptor polypeptide in gastric smooth muscle: identification of a core pentapeptide retaining full thrombin-mimetic intrinsic activity. Mol. Pharmacol., 42, 186-191.
13. HUI, K.U., JAKUBOWSKI, J.A., WYSS, V.L. & ANGLETON, E.L. (1992). Minimal sequence requirements of thrombin receptor agonist peptide. Biochem. Biophys. Res. Commun., 184, 790-796.
14. ISHIHARA, H., CONNOLLY, A.J., ZENG, D., KAHN, M.L., ZHENG, Y.W., TIMMONS, C., TRAM, T. & COUGHLIN, S.R. (1997). Protease-activated receptor-3 is a second thrombin receptor in humans. Nature, 386, 502-506.
15. KAHN, M.K., ZHENG, Y.-W., HUANG, W., BIGORNIA, V., ZENG, D., MOFF, S., FARESE, JR R.V. TAM, C. & COUGHLIN, S.R. (1998). A dual thrombin receptor system for platelet activation. Nature, 394, 690-694.
16. KAWABATA, A., SAIFEDDINE, M., AL-ANI, B., LEBLOND, L. & HOLLENBERG, M.D. (1999). Evaluation of proteinase-activated receptor-a (PAR1) agonists and antagonists using a cultured cell receptor desensitization assay: activation of PAR2 by PAR1-targeted ligands. J. Pharmacol. Exp. Ther., 288, 358-370.
17. KONG, W., MCCONALOGUE, K., KHITIN, L.M., HOLLENBERG, M.D., PAYAN, D.G., BÖHM, S.K. & BUNNETT, N.W. (1997). Luminal trypsin may regulate enterocytes through proteinase-activated receptor 2. Proc. Natl. Acad. Sci. U.S.A., 94, 8884-8889.
18. LERNER, D.J., CHEN, M., TRAM, T. & COUGHLIN, S.R. (1996). Agonist recognition by proteinase-activated receptor 2 and thrombin receptor. J. Biol. Chem., 271, 13943-13947.
19. LOPEZ, J.G., CHEW, S.J., THOMPSON, H.W., MALTER, J.S., INSLER, M.S. & BEUERMAN, R.W. (1992). EGF cell surface receptor quantitation on ocular cells by an immunocytochemical flow cytometry technique. Invest. Ophthalmol. Vis. Sci., 33, 2053-2062.
20. NEVICZ, T., ISHII, M., WANG, L., CHEN, M., CHEN, J., TURCK, C.W., COHEN, F.E. & COUGHLIN, S.R. (1995). Mechanisms of thrombin receptor agonist specificity. Chimeric receptors and complementary mutations identify an agonist recognition site. J. Biol. Chem., 270, 21619-21625.
21. NATARAJAN, S., RIEXINGER, D., PELUSO, M. & SEILER, S.M. (1995). 'Tethered ligand' derived pentapeptide agonists of thrombin receptor: a study of side chain requirements for human platelet activation and GTPase stimulation. Int. J. Pept. Protein. Res., 45, 145-151.
22. NYSTEDT, S., EMILSSON, K., WAHLESTADT, C. & SUNDELIN, J. (1994). Molecular cloning of a potential proteinase activated receptor. Proc. Natl. Acad. Sci. U.S.A., 91, 9208-9212.
23. 2+ mobilization. FEBS Lett., 288, 1223-1228.
24. SAIFEDDINE, M., AL-ANI, B., CHENG, C.-H., WANG, L. & HOLLENBERG, M.D. (1996). Rat proteinase-activated receptor-2 (Par2): cDNA sequence and activity of receptor-derived peptides in gastric and vascular tissue. Br. J. Pharmacol., 118, 521-530.
25. SCARBOROUGH, R.M., NAUGHTON, M.-A., TENG, W., HUNG, D.T., ROSE, J., VU, T.-K.H., WHEATON, V.I., TUREK, C.W. & COUGHLIN, S.R. (1992). Tethered ligand agonist peptides: structural requirements for thrombin receptor activation reveal mechanism of proteolytic unmasking of agonist function. J. Biol. Chem., 267, 13146-13149.
26. VASSALLO, J.R., KIEBER-EMMONS, T., CICHOWSKI, K. & BRASS, L.F. (1992). Structure-function relationships in the activation of platelet thrombin receptors by receptor-derived peptides. J. Biol. Chem., 267, 6081-6085.
27. VU, T.K.H., HUNG, D.T., WHEATON, V.I. & COUGHLIN, S.R. (1991). Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation. Cell, 64, 1057-1068.
28. WATSON, A.J., HOGAN, A., HAHNEL, A., WIEMER, K.E. & SCHULTZ, G.A. (1992). Expression of growth factor ligand and receptor genes in the preimplantation bovine embryo. Mol. Reprod. Dev., 31, 87-95.
29. XU, W.-F., ANDERSEN, H., WHITMORE, T.E., PRESNESS, S.R., YEE, D.P., CHING, A., GILBERT, T., DAVIE, E.W. & FOSTER, D. (1998). Cloning and characterization of human protease-activated receptor 4. Proc. Natl. Acad. Sci. U.S.A., 95, 6642-6646.
30. ZAGURSY, R.J., SHARP, D., SOLOMON, K.A. & SCHWARTZ, A. (1995). Quantitation of cellular receptors by a new immunocytochemical flow cytometry technique. BioTechniques, 18, 504-509.